Chlorpromazine was the first antipsychotic drug, used during the 1950s and 1960s. Used as chlorpromazine hydrochloride and sold under the tradenames Largactil® and Thorazine®, it has sedative, hypotensive and antiemetic properties as well as anticholinergic and antidopaminergic effects. It has also anxiolytic (alleviation of anxiety) properties. Today, chlorpromazine is considered a typical antipsychotic.
Chemistry
Chlorpromazine is derived from
phenothiazine, and has an
aliphatic side chain, typical for low to middle potency neuroleptics. The oral
bioavailability is estimated to be 30% to 50% due to extensive first pass metabolization in the liver. Its elimination-halflife is 16 to 30 hours. It has many active metabolites (approx. 75 different ones) with greatly varying halflives and own pharmacological profiles. The CYP-450
isoenzymes
1A2 and
2D6 are needed for metabolization of chlorpromazine and the subtype 2D6 is inhibited by chlorpromazine (NB: possible interactions with other drugs).
Mechanism of action
Central
More on
[ Chlorpromazine ]
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